Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1367833 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
On the basis of pharmacophoric modelling studies of existing NNRTIs, a series of isatin β-thiosemicarbazone derivatives was synthesized and evaluated for their anti-HIV activity in HTLV-IIIB strain in the CEM cell line. Three compounds showed significant anti-HIV activity, whereupon compound 6 was found to be the most active compound with an EC50 value of 2.62 μM and a selectivity index of 17.41, while not being cytotoxic to the cell line at a CC50 value of 44.90 μM. Other tested compounds exhibited marked activity below their toxicity threshold.
Graphical abstractA series of isatin β-thiosemicarbazones derivatives was synthesized and evaluated for anti-HIV activity in HTLV-IIIB strain in CEM cell line. Compound 6 was found to be the most active compound with an EC50 value of 2.62 μM.Figure optionsDownload full-size imageDownload as PowerPoint slide